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Aspirin

Overview

Aspirin is an NSAID (non-steroidal anti-inflammatory drug). It has anti-infalammatory, analgesic, antipyretic and antithrombotic activity. It interferes with prostaglandin synthesis by irreversibly inhibiting cyclooxygenase. It was synthesized in 1853, but the drug was not in use until 1899, when it was found to be effective in the arthritis and well tolerated. The name it was coined from the German word for the compound, acetylspirsaure. Because of its greater efficacy and lower cost, it rapidly replaced the natural products in use at that time, and has remained one the most widely employed remedies for over 90 years.

Category:

Primary Characterstics

Molecular Structure of Aspirin
Aspirin also known as Acetyl salicylicacid. . It is of Synthetic origin and belongs to Benzoic Acid. It belongs to Cyclo-oxygenase inhibitor pharmacological group on the basis of mechanism of action and also classified in Analgesics and Anti-inflammatory Agents and Salicylate pharmacological group.The Molecular Weight of Aspirin is 180.00.
Its pKa is 3.5.

Pharmacokinetics

Oral absorption of Aspirin is found to be 85% ±5. Volume of distribution is found to be 0.2 l/kg and plasma protien binding is 80-90%. Presystemic metabolism is noted to be 72.5% ±2.5 and metabolism is reported Hepatic. Renal Excretion accounts for major and plasma half life is 15-20 min.

Indications

Contraindications

Aspirin is contraindicated in conditions like GI ulceration,Hypoprothrombinemia,Hypersensitivity.

Drug Interactions

Aspirin is known to interact with other drugs, the details of drug interactions is as follows:

DrugDetailsSeverityOnsetManagement
Acetazolamide (Na)Aspirin displace acetazolamide from plasma protein binding site and reduce renal clearence results in severe metabolic acidosis and/or salicylate toxicity. Acetazolamide change the pH of plasma due to which amount of unionized salicylates increase which may enter in CNS result in coma and death.MajorConcomitant use should be avoided but if necessary monitor the patient`s mental status and acid base balance very carefully.
Alcohol
Alendronate (Na)
AlteplaseIncreased risk of severe bleeding in case of concomitant use.ModerateCarefully monitor signs of bleeding.
AnagrelideThe potential risks and benefits of concomitant use of anagrelide with aspirin should be assessed, particularly in patients with a high risk profile for haemorrhage, before treatment is commenced.
Corticotropin
Diflunisal
Dipyridamole
Docusate (Na)
Dorzolamide
Enalapril (Maleate)Risk of renal impairment when Aspirin (in doses over 300mg daily) given with ACE inhibitors (e.g Fosinopril), also hypotensive effects antagonized by aspirin and other NSaids by blocking prostraglandins production. the combination of aspirin with enalapril may result in nephrotoxity
EnoxaparinIn those Patients receiving enoxaparin, risk of epidural or spinal hematoma become develop which may increase by concomitant use of enoxaparin with aspirin.MajorAspirin should avoid in patients receiving enoxaparin.Strickly monitor the sign and symptoms of neurologic impairement.
EplerenoneNSAIDs may possibly reduce the antihypertensive and/or diuretic effects of potassium-sparing diuretics and may increase risk of hyperkalaemia.
Fenbufen
FlurbiprofenAspirin decreases the plasma concentration of flurbiprofen. Aspirin may displace flurbiprofen from plasma protein binding site results in increased concentration of unbound, or free, drug available for clearence.During concomitant therapy, patient should take medication with food.
Fosinopril (Na)Aspirin antagonize the hypotensive effect of fosinopril by inhibiting the synthesis of prostaglandin and thus suppressing prostaglandin mediated hemodynamic effect of fosinopril.ModerateIn case of long term therapy blood pressure and renal efficiency should monitor regularly and the lowest therapeutic dosage of aspirin should be used.
Fosinopril (Na)Risk of renal impairment when Aspirin (in doses over 300mg daily) given with ACE inhibitors (e.g Fosinopril), also hypotensive effects antagonized.
Gallopamil
Gliclazide
GlipizideHypoglycemic effect of glipizide may be potentiated by aspirin by stimiulating insulin secretion.ModerateClosely monitor the development of hypoglycaemia.
GriseofulvinGriseofulvin decreases the serum concentration of aspirin by interfering its absorptionMinorIf these drugs must be given together , staggered the dose and carefully monitor the level of salicylate.
Heparin (Na) and Heparin (Cl)Aspirin enhances anticoagulant effects of Heparin by interfering with platelet adhesion result in increased risk of bleeding.ModerateClose clinical and laboratory observation is recommended for bleeding complication.
Hirudin
Human Insulin
Hydrocortisonehydrocortisone increase the bioavailability of aspirin
IbuprofenIbuprofen bind reversibly at the active site of platelet cyclogenase and thus competitively inhibit this enzyme but because this binding is reversible so it cause temporary rather than sustained depression of thromboxane formation an thus antagonize the anti-platelet and cardioprotective effect of low-dose aspirin.MajorTake medication with food and immediately report sign and symptoms of GI ulceration and bleeding.
IndomethacinIndomethacin bind reversibly at the active site of platelet cyclogenase and thus competitively inhibit this enzyme but because this binding is reversible so it cause temporary rather than sustained depression of thromboxane formation and thus antagonize the anti-platelet and cardioprotective effect of low-dose aspirin.MajorMedications should be taken with food and report the sign and symptoms of GI ulceration and bleeding immediately.
Insulin LisproHypoglycaemic effect of insulin may be potentiated by aspirin by stimulating secretion of insulin.ModerateClosely monitor the development of hypoglycemia particularly in advanced age or renally impaired patient. Dose of insulin should be adjusted accordingly.
Iopanoic Acid
Itopride (HCl)
Ketorolac (Tromethamine)Concurrent use of ketorolac and aspirin increases the risk of aspirin adverse effects.MajorCoadministration of these agents is considered contraindicated.
MeclofenamateConcurrent administration of aspirin may lower meclofenamate sodium plasma levels, possibly by competing for protein-binding sites. The urinary excretion of meclofenamate sodium is unaffected by aspirin, indicating no change in meclofenamate sodium absorption. Meclofenamate sodium does not affect serum salicylate levels. Greater fecal blood loss results from concomitant administration of both drugs than from either drug alone.
MethazolamideCo-administration may lead to anorexia,lethargy,coma and death.
Methohexitone (Na)
MethotrexateAspirin reduces the renal elimination of methotrexate and may displace it from binding site, thus increase the pharmacological effect and toxicity of methotrexate.MajorClosely monitor the sign and symptoms of bone marrow suppression and nephrotoxicity.
MethylprednisoloneMethyl prednisolone decreases the serum concentration and thus therapeutic effects of salicylates by increaseing renal clearence and inducing hepatic metabolism.ModerateMedications should be taken with food and immediately report the sign and symptoms of GI ulceration and bleeding.
Methylprednisolone
Metoclopramide (HCl)
Metoprolol (Tartrate)High doses of salicylates alter the antihypertensive effect of beta-blockers by inhibiting the synthesis of prostaglandinMinorMonitor the altered antihypertensive response whenever salicylate is introduced or discontinued.
Mifepristone
MoexiprilAspirin reduces the hypotensive effect of moexipril by inhibiting prostaglandin synthesis and thus suppressing the prostaglandin mediated hemodynamic effect of moexipril.ModerateMonitor blood pressure regularly and lowest therapeutic dose of aspirin should be used.
Nadroparin (Ca)Concurrent use may increase the risk of hemorrhage.
Nefopam (HCl)ADVICE: Avoid concomitant use of Aspirin with NSAIDs (increased risk of side effects).
Nicoumalone
NizatidineIn patients given very high doses (3,900 mg) of aspirin daily, increases in serum salicylate levels were seen when nizatidine, 150 mg b.i.d., was administered concurrently.
Oligomeric ProcyanidinConcurrent use of high doses of OPCs with Aspirin might cause a risk of excessive bleeding.
Pentoxifylline
Phenoxymethylpenicillin (K)
Phenylbutazone Coadministration exacerbate the serious gastrointestinal toxicity. Aspirin at higher doses also decreases the plasma concentration of phenylbutazoneModerateCoadministration should be avoided due to increased risk of toxicity. Patient should take medication with food and should report the sign and symptoms of GI ulceration and bleeding to physician immediately.
Phenytoin (Na)Aspirin enhances effects of Phenytoin.
PiroxicamCombined use of aspirin with piroxicam aggravate gastrointestinal toxicity. aspirin at higher doses decrease the plasma concentration of piroxicam. ADVICE: Avoid concomitant use of Aspirin with NSAIDs (increased risk of side effects). ModerateDuring concomitant therapy, patient should take medication with food and should immediately report to physician about sign and symptoms of GI ulceration and bleeding.
Piroxicam-beta-cyclodextrinThe concomitant use of aspirin and piroxicam produces reduction in the plasma level of Piroxicam
Porcine Insulin
ProbenecidHigh doses of aspirin inhibit the uricosuric effect of probenecid. Aspirin antagonizes effects of probenecid.Minor
Protirelin
ReteplaseConcurrent use may increase the risk of bleeding.
Reviparin SodiumAspirin may potentiate the action of Reviparin.
RimantadinePeak plasma concentrations and AUC of rimantadine were reduced approximately 10% in the presence of aspirin.
RofecoxibConcomitant administration of low-dose aspirin with Rofecoxib may result in an increased rate of GI ulceration or other complications.
SalsalateSalsalate, like aspirin, is converted to salicylic acid. Therefore, adding aspirin to salsalate can cause salicylic acid toxicity.
SaruplaseSaruplase in combination with aspirin can be given safely to acute myocardial infarction patients.
Sodium AcetateAgents that cause urinary alkalinization can reduce serum salicylate concentrations in patients receiving anti-inflammatory dosages of aspirin. The mechanism involves reduction in salicylate renal tubular reabsorption due to increased urinary pH, resulting in increased renal salicylate clearance especially above urine pH of 7. This interaction is sometimes exploited in the treatment of salicylate toxicity.ModeratePatients treated chronically with urinary alkalinizers and large doses of salicylates (i.e. 3 g/day or more) should be monitored for potentially diminished or inadequate analgesic and anti-inflammatory effects, and the salicylate dosage adjusted if necessary.
Sodium Valproate
StreptokinaseIncreased risk of bleeding.ModerateCarefully monitor the signs of bleeding, during coadministration.
SulindacAspirin decreases the plasma concentration of sulindac. Aspirin may displace sulindac from plasma protein binding site results in increased concentration of unbound, or free, drug available for clearence.ModerateDuring concomitant therapy, patient should take medication with food.
SulphinpyrazoneAspirin antagonizes effects of Sulphinpyrazone.
TenecteplaseAspirin may increase the risk of bleeding if administered prior to, during or after Tenecteplase therapy.
Thiopentone (Na)
Tiaprofenic AcidAspirin can cause an increased risk of bleeding.
Tienilic Acid
UrokinaseIncreased risk of severe bleeding.ModerateDuring coadministration, carefully monitor the signs of bleeding.
Varicella Vaccine
VilazodoneNSaids, increase risk of bleedingcareful monitoring should be instituted
Warfarin (Na)Aspirin may enhance the anticoagulant effect of Warfarin and thus increase the risk of bleeding by inhibiting platelet aggregation.MajorPatients receiving Warfarin should not take Aspirin on an as-needed basis. Nonacetylated salicylates might be safer than Aspirin. Acetaminophen (<1.3 g/day for <1 week) is usually a good antipyretic and analgesic choice for patients taking Warfarin. Caution with higher doses.1 Aspirin (80-325 mg/day) and Warfarin are used together, in selected cases and with careful monitoring, for the prevention of cardiovascular events. Monitor for increased signs and symptoms of bleeding if Warfarin and Aspirin are used concomitantly. Aspirin doses > 325 mg/day may require more frequent INR monitoring.
ZafirlukastAspirin increases plasma concentration of leukotriene antagonists (e.g Zafirlukast).
Zidovudine

These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Interference in Pathology

  • Urine tests for Catecholamines, dopa, glucose, ketones, hippuric acid
  • Pregnancy tests carried out on urine
  • Plasma/Serum tests for albumin, barbiturates, calcium, propylthiouracil, tyrosine & uric acid
  • Thyroid Function Test
  • Urine tests for homogentisic acid & homavanillic acid
  • Urine tests for 17-hydroxycorticosteroids & 5-hydroxyindoleacetic acid.
  • hippuric acid,, serum / plasma albumin, calcium, propylthiouracil, tyrosine and uric acid

Side Effects

The severe or irreversible adverse effects of Aspirin, which give rise to further complications include Urticaria, Gi bleeding, Rhinitis, Angioneurotic edema, Hepatitis, Hepatomegaly.

Aspirin produces potentially life-threatening effects which include Cerebral hemorrhage, Airway obstruction, Gastric ulceration, Gastric erosion. which are responsible for the discontinuation of Aspirin therapy.

The signs and symptoms that are produced after the acute overdosage of Aspirin include Coma, Acidosis, Hyperthermia, Volume depletion, Hyperglycemia, Renal failure, Hyperventilation, Cardiovascular collapse, Vertigo, Tinnitus, Hyperkalemia.

The symptomatic adverse reactions produced by Aspirin are more or less tolerable and if they become severe, they can be treated symptomatically, these include Dizziness, Vertigo, Nausea, Vomiting, Tinnitus, Epigastric discomfort, Dyspepsia, Asthma, Respiratory alkalosis, Bleeding.

Available Brands

Click on the appropriate strength of the dosage form to view its available brands.

Single Ingredient

Tabs: 75 mg, 100 mg, 150 mg, 300 mg, 500 mg,

Multi ingredient

Tabs: 75 mg, 150 mg, 300 mg, 385 mg,

Dosage

Aspirin's dosage details are as follows:
Dose Single Dose Frequency Route Instructions

Adult Dosage

0 to 45 mg/kg/d22 (22.5)As recommended.POfor inflammation
75 to 325 mg200 (200)1 hourlyPOProphylaxis of MI, stable angina, and cerebro-vascular disease.
300 to 900 mg600 (600)4 hourlyPOMild to moderate pain, pyrexia, migraine, and dysmenorrhea.
600 to 900 mg750 (750)4 hourlysuppositoriesupto 3.6g

Paedriatic Dosage ( 20 Kg. )

50 to 75 mg/kg62 (62.5)6 hourlyOralAs Required

Neonatal Dosage ( 3 Kg. )

No data regarding the neonatal dosage details of Aspirin is available.

High Risk Groups

Drug should not be given to Paediatrics, Pregnant Mothers, patients suffering from Kidney dysfunction, patients suffering from Liver Malfunction, and Neonates.

If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.

Warning / Precautions

Aspirin should be used with caution in patients with chronic renal insufficiency, gastric ulcer, severe anemia, and patients intolerant to salicylate. Avoid aspirin in patient with history of blood coagulation defects and if patient taking anticoagulants. Liver function should be monitored in patients receiving large doses of aspirin or in patients with pre-existing hepatic disease in order to prevent reversible, dose dependent hepatotoxicity.

Storage Conditions

Suppositories

Store in a well closed container. Refrigeration is recommended. Do not Freeze. Protect from Sunlight and Moisture.

Tab

Store in a well closed container, Below 40°C. Protect from Sunlight and Moisture.

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